Microwave assisted synthesis of some novel acetazolamide cyclocondensed 1,2,3,4-tetrahydropyrimidines as a potent antimicrobial and cytotoxic agents

Abstract

A new series of some novel acetazolamide cyclocondensed 1,2,3,4-tetrahydropyrimidines was prepared by reacting of N-{[5-(acetylamino)-1,3,4-thiadiazol-2-yl]sulfonyl}-3-oxobutanamide with urea/thiourea and appropriate aldehyde in the presence of catalytic amount of laboratory made p-toluenesulfonic acid as an efficient catalyst. Confirmation of the chemical structure of the synthesized compounds (12a–n) was substantiated by TLC, different spectral data IR, 1H NMR, Mass spectra and elemental analysis were done. The synthesized compounds were evaluated for in-vitro antimicrobial and cytotoxicity against Bacillus subtilis, Escherichia coli and Vero cells. The titled compounds exhibited weak, moderate, or high in-vitro antimicrobial and cytotoxicity. Compounds 12c, 12d, 12g and 12h, exhibited potential antimicrobial and in-vitro cytotoxicity.

Keywords

• Acetazolamide
• Tetrahydropyrimidines
• Cyclocondensation
• Antimicrobial
• Cytotoxicity